- Compounds and compositons for treating C1s-mediated diseases and conditions
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Disclosed is a method for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of Formula I or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R1, R2, R3, R4, X, Y and Z are defined in the specification.
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- Structure-Based design, synthesis and SAR of a novel series of thiopheneamidine urokinase plasminogen activator inhibitors
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The serine protease urokinase plasminogen activator (uPA) is thought to play a central role in tumor metastasis and angiogenesis. Molecular modeling studies suggest that 5-thiomethylthiopheneamidine inhibits uPA by binding at the S1 pocket of the active site. Further structure based elaboration of this residue resulted in a novel class of potent and selective inhibitors of uPA.
- Subasinghe, Nalin L.,Illig, Carl,Hoffman, James,Rudolph,Wilson, Kenneth J.,Soll, Richard,Randle, Troy,Green, David,Lewandowski, Frank,Zhang, Marie,Bone, Roger,Spurlino, John,DesJarlais, Renee,Deckman, Ingrid,Molloy, Christopher J.,Manthey, Carl,Zhou, Zhau,Sharp, Celia,Maguire, Diane,Crysler, Carl,Grasberger, Bruce
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p. 1379 - 1382
(2007/10/03)
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- Heteroaryl amidines, methylamidines and guanidines, preparation thereof, and use thereof as protease inhibitors
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The present invention is directed to compounds of Formula I: wherein X is O, S or NR7and R1-R7, Y and Z are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, plasmin and urokinase. Certain of the compounds exhibit direct, selective inhibition of urokinase, or are intermediates useful for forming compounds having such activity.
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